title: HIV-1 inhibiting capacity of novel forms of presentation of GB virus C peptide domains is enhanced by coordination to gold compounds.
abstract: Following the report of beneficial effects of co-infection by GB virus C (GBV-C) for HIV-infected patients, we have studied synthetic GBV-C peptides and their relationship with HIV type-1. This paper reports the design and synthesis of new forms of presentation of two peptide inhibitors corresponding to the envelope proteins E1 and E2 of GBV-C, together with a study of their anti-HIV-1 activity. Homogeneous and heterogeneous multiple antigenic peptides (MAPs), lipophilic derivatizations, cyclization and peptide-gold conjugations are the chemical design strategies adopted. Our aim is to enhance the anti-viral potency of the GBV-C peptide domains. Of all the GBV-C peptide derivatives studied, peptide-gold complexes derived from the (22-39) sequence of the GBV-C E1 protein were the most active entry inhibitors. These results support the putative modulation of HIV-1 infection by the GBV-C E1 protein and open new perspectives for the development of novel peptide-derived HIV-1 entry inhibitors.
authors.affiliation: Unit of Synthesis and Biomedical Applications of Peptides, IQAC-CSIC, Spain. isabel.haro@iqac.csic.es.
authors.forename: María J
authors.initials: MJ
authors.lastname: Gómara
authors.forename: Ramona
authors.initials: R
authors.lastname: Galatola
authors.forename: Alejandro
authors.initials: A
authors.lastname: Gutiérrez
authors.forename: María C
authors.initials: MC
authors.lastname: Gimeno
authors.forename: José M
authors.initials: JM
authors.lastname: Gatell
authors.forename: Víctor
authors.initials: V
authors.lastname: Sánchez-Merino
authors.forename: Eloísa
authors.initials: E
authors.lastname: Yuste
authors.forename: Isabel
authors.initials: I
authors.lastname: Haro
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D029407:GB virus C / Q000737:chemistry*; D017612:Gold Compounds / Q000737:chemistry*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D017612:Gold Compounds; D010455:Peptides